maraviroc 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definition	Drug id	CAS RN
antivirals CCR5 (Chemokine CC motif receptor 5) receptor antagonists	1635	376348-65-1

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: MD6P741W8A UK-427857 maravirok marawirok maraviroc celsentri selzentry	Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc. Molecular weight: 513.68 Formula: C29H41F2N5O CLOGP: 3.26 LIPINSKI: 1 HAC: 6 HDO: 1 TPSA: 63.05 ALOGS: -4.68 ROTB: 8 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

MD6P741W8A
UK-427857
maravirok
marawirok
maraviroc
celsentri
selzentry

Maraviroc is a member of a therapeutic class called CCR5 co-receptor antagonists. Maraviroc selectively binds to the human chemokine receptor CCR5 present on the cell membrane, preventing the interaction of HIV-1 gp120 and CCR5 necessary for CCR5-tropic HIV-1 to enter cells. CXCR4-tropic and dual-tropic HIV-1 entry is not inhibited by maraviroc.

Molecular weight: 513.68
Formula: C29H41F2N5O
CLOGP: 3.26
LIPINSKI: 1
HAC: 6
HDO: 1
TPSA: 63.05
ALOGS: -4.68
ROTB: 8

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
0.60	g	O

ADMET properties:

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Property	Value	Reference
CL (Clearance)	9.40 mL/min/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	8 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	33.37 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	23 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
Vd (Volume of distribution)	2.30 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	12.80 hours	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.25 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
Aug. 6, 2007	FDA	VIIV HLTHCARE

FDA Adverse Event Reporting System (Female)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Pathogen resistance	89.69	58.08	20	817	6378	63481807
Virologic failure	87.85	58.08	16	821	1846	63486339
Exposure during pregnancy	75.77	58.08	38	799	155509	63332676
Viral mutation identified	75.39	58.08	14	823	1796	63486389
Abortion spontaneous	68.32	58.08	25	812	47170	63441015
Lipodystrophy acquired	65.39	58.08	12	825	1440	63486745

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FDA Adverse Event Reporting System (Male)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Virologic failure	283.55	26.57	61	2136	3419	34951315
Viral mutation identified	219.35	26.57	48	2149	2906	34951828
Pathogen resistance	104.35	26.57	34	2163	9448	34945286
Drug resistance	99.76	26.57	43	2154	25884	34928850
Immune reconstitution inflammatory syndrome	63.51	26.57	23	2174	8736	34945998
Blood HIV RNA increased	53.74	26.57	13	2184	1217	34953517
CSF HIV escape syndrome	43.63	26.57	8	2189	193	34954541
Progressive multifocal leukoencephalopathy	43.50	26.57	18	2179	9746	34944988
Viral load increased	40.09	26.57	12	2185	2515	34952219
Hodgkin's disease	31.86	26.57	8	2189	873	34953861

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FDA Adverse Event Reporting System (Geriatric)

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MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Virologic failure	298.69	30.48	58	2331	4133	79737866
Viral mutation identified	248.05	30.48	49	2340	3809	79738190
Pathogen resistance	146.67	30.48	41	2348	14301	79727698
Drug resistance	106.74	30.48	42	2347	42171	79699828
Immune reconstitution inflammatory syndrome	73.93	30.48	24	2365	13817	79728182
CSF HIV escape syndrome	72.66	30.48	12	2377	335	79741664
Viral load increased	67.33	30.48	16	2373	2932	79739067
Drug interaction	47.33	30.48	60	2329	415123	79326876
Lipodystrophy acquired	47.08	30.48	13	2376	4312	79737687
Progressive multifocal leukoencephalopathy	46.80	30.48	19	2370	20581	79721418

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	J05AX09	ANTIINFECTIVES FOR SYSTEMIC USE ANTIVIRALS FOR SYSTEMIC USE DIRECT ACTING ANTIVIRALS Other antivirals
CHEBI has role	CHEBI:36044	antiviral drugs
CHEBI has role	CHEBI:59886	HIV fusion inhibitors
CHEBI has role	CHEBI:63673	CCR5 antagonist
FDA EPC	N0000175572	CCR5 Co-receptor Antagonist
FDA MoA	N0000175445	Chemokine Co-receptor 5 Antagonists
MeSH PA	D019380	Anti-HIV Agents
MeSH PA	D000890	Anti-Infective Agents
MeSH PA	D044966	Anti-Retroviral Agents
MeSH PA	D000998	Antiviral Agents

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Drug Use | Suggest Off label Use Form| |View source of the data|

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Disease	Relation	SNOMED_ID	DOID
CCR5 Tropic Drug Resistant HIV Infection	indication
Myocardial infarction	contraindication	22298006	DOID:5844
Orthostatic hypotension	contraindication	28651003
Infectious disease	contraindication	40733004
Viral hepatitis C	contraindication	50711007	DOID:1883
Acute nephropathy	contraindication	58574008
Chronic type B viral hepatitis	contraindication	61977001
Chronic renal failure syndrome	contraindication	90688005
Kidney disease	contraindication	90708001	DOID:557
Disease of liver	contraindication	235856003	DOID:409

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	8.8	Basic
pKa2	5.07	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

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Formulation strength	Trade name	Applicant	Application number	Approval date	Type	Dose form	Route	Exclusivity date	Description
20MG/ML	SELZENTRY	VIIV HLTHCARE	N208984	Nov. 4, 2016	RX	SOLUTION	ORAL	Oct. 30, 2023	NEW PATIENT POPULATION
20MG/ML	SELZENTRY	VIIV HLTHCARE	N208984	Nov. 4, 2016	RX	SOLUTION	ORAL	April 30, 2024	PEDIATRIC EXCLUSIVITY

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Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
C-C chemokine receptor type 5	GPCR	P51681	CCR5_HUMAN	ANTAGONIST	Kd	7.60	CHEMBL	CHEMBL
Multidrug and toxin extrusion protein 1	Transporter	Q96FL8	S47A1_HUMAN		IC50	4.76	CHEMBL
C-C chemokine receptor type 5	GPCR		CCR5_MOUSE		IC50	8.28	CHEMBL
C-C chemokine receptor type 5	GPCR		CCR5_MACMU		Ki	9.62	CHEMBL

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External reference:

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ID	Source
012282	NDDF
118030	MMSL
24072	MMSL
3002977	PUBCHEM_CID
356432	MMSL
4026629	VUID
4026629	VANDF
427805000	SNOMEDCT_US
429603001	SNOMEDCT_US
620216	RXNORM

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Maraviroc	HUMAN PRESCRIPTION DRUG LABEL	1	31722-579	TABLET, FILM COATED	150 mg	ORAL	ANDA	27 sections
Maraviroc	HUMAN PRESCRIPTION DRUG LABEL	1	31722-580	TABLET, FILM COATED	300 mg	ORAL	ANDA	27 sections
Maraviroc	HUMAN PRESCRIPTION DRUG LABEL	1	72865-231	TABLET, FILM COATED	150 mg	ORAL	ANDA	31 sections
Maraviroc	HUMAN PRESCRIPTION DRUG LABEL	1	72865-232	TABLET, FILM COATED	300 mg	ORAL	ANDA	31 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-223	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-223	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-223	TABLET, FILM COATED	150 mg	ORAL	NDA	30 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-224	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-224	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections
SELZENTRY	HUMAN PRESCRIPTION DRUG LABEL	1	49702-224	TABLET, FILM COATED	300 mg	ORAL	NDA	30 sections

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